Novocaine

General characteristics. Structure:

Active ingredient: 2,5 g or 5 g of novocaine.

Excipients: acid solution of hydrochloric 0,1 M - to рН 3,8 - 4,5, water for injections.

Novocaine has the moderate anesthetizing activity and big width of therapeutic action.

Pharmacological properties:

Pharmacodynamics. Novocaine has the moderate anesthetizing activity and big width of therapeutic action. Blocks natrium channels and thus interferes with generation of impulses in the terminations of sensory nerves and to carrying out impulses on nerve fibrils. Suppresses carrying out not only painful, but also impulses of other modality.

At resorptive action has the oppressing effect on the central nervous system, weakens a spasm of smooth muscles, possesses ganglioblokiruyushchy action, in high doses can break neuromuscular conductivity. Novocaine has hypotensive and antiarrhythmic effect (reduces excitability and automatism, worsens conductivity).

In comparison with lidocaine and bupivacaine, novocaine has less expressed anesthetic effect, has rather small toxicity and bigger therapeutic width. In an organism drug is hydrolyzed by esterases of a blood plasma and fabrics with formation of two main metabolites: diethylaminoethanol and paraaminobenzoic acid (is    an antagonist    of sulfanamide    chemotherapeutic    drugs). Metabolites are allocated with kidneys.

Indications to use:

Apply to a local infiltration anesthesia, at various surgical interventions. For carrying out novocainic blockade - perinephric and vagosympathetic. For carrying out - circulator and juxtaspinal blockade at eczema, neurodermatitis, a sciatica and other painful states. For  removal  of spasms  of peripheral  vessels  and  improvement  of microcirculation  at freezing injuries (in the doreaktivny period).

Route of administration and doses:

For an infiltration anesthesia solutions use 0,25 - 0,5%; anesthesia by A. V. Vishnevsky's method (hard creeping infiltration) - 0,125 - 0,25% solutions. At local anesthesia for reduction of absorption and increase in duration of action add 0,1% to solution of novocaine Adrenalinum hydrochloricum solution at the rate of 1 drop on 2 - 5 - 10 ml of solution of novocaine. At perinephric blockade by A. V. Vishnevsky's method enter into pararenal cellulose on 50 - 80 ml 0,5% of solution or 100 - 150 ml of 0,25% of solution of novocaine.

For carrying out circulator and juxtaspinal blockade at eczema, neurodermatitis, a sciatica enter 0,25 - 0,5% novocaine solution.  

Intravenously enter from 1 to 10 - 15 ml of 0,25 - 0,5% of solution; enter slowly, better in isotonic solution of sodium chloride. The quantity of injections (sometimes to 10 - 20) depends on disease severity. The highest doses: at intramuscular introduction of 0,1 g (5 ml of 2% of solution), (20 ml 0,5%rastvora); For an infiltration anesthesia the highest doses: the first single dose at the beginning of operation - no more than 1,25 g when using 0,25% of solution (500 ml) and 0,75 g at use of 0,5% of solution (150 ml). Further for each hour of operation - no more than 2,5 g when using 0,25% of solution (1000 ml) and 2 g at use of 0,5% of solution (400 ml).

For removal of spasms of peripheral vessels and improvement of microcirculation at freezing injuries, the mix consisting of 10 ml of 0,25% of solution of novocaine, 2 ml of 2% of solution of a papaverine, 2 ml of 1% of acid solution of nicotinic and 10000 PIECES of heparin is used. It is entered vnutriarterialno slowly.

Features of use:

It is necessary to consider that when carrying out local anesthesia at use of the same dose toxicity of novocaine of subjects is higher, than the applied solution is more concentrated.

Novocaine slowly gets through the unimpaired mucous membranes therefore it is a little effective for poverkhnostony anesthesia.

Pregnancy and period of feeding by a breast. During the periods of pregnancy and feeding by a breast drug should be used with extra care, according to absolute indications.

Side effects:

From warmly vascular system - arterial hypotension, a collapse.

From TsNS – weakness, dizziness.

Allergic reactions – a small tortoiseshell, development of an acute anaphylaxis is possible.

Interaction with other medicines:

Novocaine strengthens the oppressing action on TsNS of anesthetics, hypnotic drugs, sedative drugs, narcotic analgetics and anxiolytics.

The metabolite of PABK Novocaine inhibits effect of streptocides.

Contraindications:

Hypersensitivity to drug. Children up to 12 years.

Overdose:

At overdose coma develops, spasms are possible.

First aid at overdose – maintenance of lung ventilation, disintoxication and symptomatic therapy.

Storage conditions:

List B. In the place protected from light, at the room temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

2,5 mg/ml solution for injections in bottles for blood substitutes on 200 ml and 400 ml. 5 mg/ml solution for injections in bottles for blood substitutes on 200 ml and 400 ml. On 28 bottles a dose of 200 ml and 15 bottles a dose of 400 ml respectively, in boxes from corrugated fibreboard (with laying and lattices).